| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
Fosaprepitant dimeglumine (also known as L-758298 dimeglumine; MK0517 dimeglumine) is a neurokinin-1 receptor antagonist for the prevention of chemotherapy-induced nausea and vomiting. Fosaprepitant is injected intravenously as an antiemetic medication. Merck & Co. created fosaprepitant, which was authorized as an Aprepitant prodrug. It helps to prevent both acute and delayed nausea and vomiting brought on by chemotherapy. Aprepitant, the active moiety, is a substrate, inducer, and inhibitor of CYP3A4, while fosaprepitant is a weak inhibitor of CYP3A4.
| Targets |
Neurokinin-1 receptor
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|---|---|
| ln Vitro |
Fosaprepitant (MK-0517, L-758,298) is a phosphoryl prodrug for aprepitant. A corticosteroid and a 5-HT 3 receptor antagonist are approved as combination therapies with the selective substance P (NK-1 receptor) antagonist aprepitant to prevent acute and delayed chemotherapy-induced nausea and vomiting. [1]
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| ln Vivo |
Fosaprepitant is intravenously administered and within 30 minutes, transforms into an aprepitant due to the action of ubiquitous phosphatases. Fosaprepitant has a well-tolerated maximum dosage of 150 mg (1 mg/ml), and its AUC for Fosaprepitant 115 mg and Aprecipitant 125 mg are bioequivalent. On day 1 of a 3-day oral aprepitant regimen, fosaprepitant 115 mg has been submitted for FDA approval as an alternative. On days 2 and 3, oral aprepitant is administered. [1]
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| References |
| Molecular Formula |
C37H56F7N6O16P
|
|---|---|
| Molecular Weight |
1004.8337
|
| Exact Mass |
1004.34
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| Elemental Analysis |
C, 44.23; H, 5.62; F, 13.23; N, 8.36; O, 25.48; P, 3.08
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| CAS # |
265121-04-8
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| Related CAS # |
Fosaprepitant; 172673-20-0; Fosaprepitant-d4 dimeglumine
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| Appearance |
White solid powder
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| SMILES |
C[C@H](C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)O[C@@H]2[C@@H](N(CCO2)CC3=NN(C(=O)N3)P(=O)(O)O)C4=CC=C(C=C4)F.CNC[C@@H]([C@H]([C@@H]([C@@H](CO)O)O)O)O.CNC[C@@H]([C@H]([C@@H]([C@@H](CO)O)O)O)O
|
| InChi Key |
VRQHBYGYXDWZDL-OOZCZQCLSA-N
|
| InChi Code |
InChI=1S/C23H22F7N4O6P.2C7H17NO5/c1-12(14-8-15(22(25,26)27)10-16(9-14)23(28,29)30)40-20-19(13-2-4-17(24)5-3-13)33(6-7-39-20)11-18-31-21(35)34(32-18)41(36,37)38;2*1-8-2-4(10)6(12)7(13)5(11)3-9/h2-5,8-10,12,19-20H,6-7,11H2,1H3,(H,31,32,35)(H2,36,37,38);2*4-13H,2-3H2,1H3/t12-,19+,20-;2*4-,5+,6+,7+/m100/s1
|
| Chemical Name |
[3-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholin-4-yl]methyl]-5-oxo-4H-1,2,4-triazol-1-yl]phosphonic acid;(2R,3R,4R,5S)-6-(methylamino)hexane-1,2,3,4,5-pentol
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| Synonyms |
MK0517; MK 0517; MK-0517; Fosaprepitant dimeglumine; Emend; Inemend
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product is not stable in solution, please use freshly prepared working solution for optimal results. (2). Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: ~50 mg/mL (~49.8 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (99.52 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9952 mL | 4.9760 mL | 9.9519 mL | |
| 5 mM | 0.1990 mL | 0.9952 mL | 1.9904 mL | |
| 10 mM | 0.0995 mL | 0.4976 mL | 0.9952 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05755659 | Recruiting | Drug: Fosaprepitant Dimeglumine for Injection |
Neoplasms | Xijing Hospital | July 15, 2022 | Not Applicable |
| NCT01504711 | Completed | Drug: fosaprepitant dimeglumine | Gastrointestinal Cancer Nausea Post Chemotherapy |
Philip Philip | June 2012 | Not Applicable |
| NCT04054193 | Completed | Drug: Fosaprepitant Dimeglumine Drug: Dexamethasone |
Chemotherapy-induced Nausea and Vomiting |
Merck Sharp & Dohme LLC | September 9, 2019 | Phase 4 |
| NCT01074697 | Completed | Drug: Fosaprepitant dimeglumine Drug: Placebo |
Nausea Vomiting |
Odense University Hospital | April 2010 | Phase 3 |
| NCT01594749 | Completed | Drug: Dexamethasone Drug: Ondansetron |
Chemotherapy-Induced Nausea and Vomiting (CINV) |
Merck Sharp & Dohme LLC | September 24, 2012 | Phase 3 |
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